更新于：2024-12-06
Cefotiam hexetil hydrochloride
盐酸头孢替安酯
更新于：2024-12-06
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构
分子式C27H39Cl2N9O7S3 |
InChIKeyFFSANQNELHESQJ-LWBICVDYSA-N |
CAS号95789-30-3 |
关联
5
项与 盐酸头孢替安酯 相关的临床试验盐酸头孢替安酯片治疗轻、中度呼吸和泌尿系统急性细菌感染的 随机、双盲、阳性药平行对照、多中心临床试验
评价盐酸头孢替安酯片人体生物等效性的单中心，开放，随机，双交叉试验
盐酸头孢替安酯片人体药代动力学试验
100 项与 盐酸头孢替安酯 相关的临床结果
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100 项与 盐酸头孢替安酯 相关的转化医学
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100 项与 盐酸头孢替安酯 相关的专利（医药）
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25
项与 盐酸头孢替安酯 相关的文献（医药）2023-07-01Redox biology
Development of an assay pipeline for the discovery of novel small molecule inhibitors of human glutathione peroxidases GPX1 and GPX4
Article
作者: Cheng, Qing ; Klumpp-Thomas, Carleen ; Hall, Matthew D ; Cheff, Dorian M ; Travers, Jameson ; Arnér, Elias S J ; Shen, Min ; Guo, Hui
Selenoprotein glutathione peroxidases (GPX), like ubiquitously expressed GPX1 and the ferroptosis modulator GPX4, enact antioxidant activities by reducing hydroperoxides using glutathione. Overexpression of these enzymes is common in cancer and can be associated with the development of resistance to chemotherapy. GPX1 and GPX4 inhibitors have thus shown promise as anti-cancer agents, and targeting other GPX isoforms may prove equally beneficial. Existing inhibitors are often promiscuous, or modulate GPXs only indirectly, so novel direct inhibitors identified through screening against GPX1 and GPX4 could be valuable. Here, we developed optimized glutathione reductase (GR)-coupled GPX assays for the biochemical high-throughput screen (HTS) of almost 12,000 compounds with proposed mechanisms of action. Initial hits were triaged using a GR counter-screen, assessed for isoform specificity against an additional GPX isoform, GPX2, and were assessed for general selenocysteine-targeting activity using a thioredoxin reductase (TXNRD1) assay. Importantly, 70% of the GPX1 inhibitors identified in the primary screen, including several cephalosporin antibiotics, were found to also inhibit TXNRD1, while auranofin, previously known as a TXNRD1 inhibitor, also inhibited GPX1 (but not GPX4). Additionally, every GPX1 inhibitor identified (including omapatrilat, tenatoprazole, cefoxitin and ceftibuten) showed similar inhibitory activity against GPX2. Some compounds inhibiting GPX4 but not GPX1 or GPX2, also inhibited TXNRD1 (26%). Compounds only inhibiting GPX4 included pranlukast sodium hydrate, lusutrombopag, brilanestrant, simeprevir, grazoprevir (MK-5172), paritaprevir, navitoclax, venetoclax and VU0661013. Two compounds (metamizole sodium and isoniazid sodium methanesulfate) inhibited all three GPXs but not TXNRD1, while 2,3-dimercaptopropanesulfonate, PI4KIII beta inhibitor 3, SCE-2174 and cefotetan sodium inhibited all tested selenoproteins (but not GR). The detected overlaps in chemical space suggest that the counter screens introduced here should be imperative for identification of specific GPX inhibitors. With this approach, we could indeed identify novel GPX1/GPX2- or GPX4-specific inhibitors, thus presenting a validated pipeline for future identification of specific selenoprotein-targeting agents. Our study also identified GPX1/GPX2, GPX4 and/or TXNRD1 as targets for several previously developed pharmacologically active compounds.
2013-05-01Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition
[Determination of unknown impurities in cefotiam hexetil by HPLC-MS/MS].
Article
作者: Zhan, Lan-Fen ; Ye, Yi ; Wang, Zhi-Hui ; Liu, Ming-Dong ; Tang, Qun-Xing ; Liao, Lin-Chuan ; Yan, You-Yi
OBJECTIVE:
To detect unknown impurities in raw drug material of cefotiam hexetil.
METHODS:
High performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was employed for the determination of impurities in cefotiam hexetil. Agilent SB-C18 column (150 mm x 2.1 mm i. d. , 3.5 microm particles) was used for chromatographic separations of cofotiam hexetil dissolved in deionized water, with mobile phase consisting of (A) 0.1% formic acid and (B) acetonitrile and timed gradient program T (min)/B (%): 0/3, 5/3, 15/20, 20/40, 30/60, 40/80. The flow rate was set at 0. 3 mL/min with DAD detector wavelength fixed at 254 nm. Electrospray ionization source was applied and operated in positive ion MRM mode. The source voltage was kept at 4 kV and cone voltage was 100 V with the mass range m/z 50-1000. Nitrogen was used as nebulizing gas and the nebulizer pressure was 40 psi. The drying gas temperature was 350 degrees C and the drying gas flow was 10 L/min. Results Unknown impurities of cefotiam hexetil were identified. Substance 1 was delta3-isomer of cefotiam hexetil. The structures of 3 other substances were also determined.
CONCLUSION:
The method is sensitive, rapid and credible for the analysis of cefotiam hexetil and its related impurities, which can be applied in quality control of cefotiam hexetil.
2013-01-01Nihon Jinzo Gakkai shi
[A case of tuberculous peritonitis in a hemodialysis patient revealed by severe diarrhea and stomachache].
Article
作者: Sawada, Katsunori ; Hara, Masayuki ; Hatta, Tsuguru ; Segawa, Hiroyoshi ; Ueno, Risa ; Ohtani, Mai
A 53-year-old woman was admitted to our hospital due to abdominal pain, diarrhea, and shunt occlusion caused by dehydration. She had undergone hemodialysis due to diabetic nephropathy over a ten-year period. She was hospitalized again with fever and a persistent high serum CRP level. We started antibiotic administration using cefotiam hexetil hydrochloride because of ascites and peritoneum thickening observed by abdominal computed tomography. Although her symptoms, such as abdominal pain and diarrhea, improved after the administration of antibiotics, the ascites and the peritoneum thickening did not improve. On the fourth hospital day, we attempted ascites aspiration to investigate the etiology of the peritonitis. Cytological examination suggested tuberculous peritonitis because of predominant macrophage cell proliferation, a high level of ADA concentration, and a high level of CA125 of ascites. Although QuantiFERON-tuberculosis (QFT) and the Gaffky scale were negative, we started multidrug therapy (isoniazid + rifampicin + pyrazinamide + ethambutol) on the 20th hospital day. She was finally diagnosed as mycobacterium tuberculous peritonitis based on biopsy of the tissue of the ileum and the results of colonoscopy. Administration of antituberculosis chemotherapy improved abdominal fullness and ascites and the patient was discharged on the 97th hospital day. Moreover Kuno et al. reported that serum soluble interleukin-2 receptor(sIL-2R) and CA-125 levels can be used to monitor the response to anti-tuberculosis treatment. In this case, we use these markers to monitor the response to treatment. We experienced a case of tuberculous peritonitis undergoing hemodialysis. Tuberculosis should be suspected when patients undergoing dialysis have long-term fever of unknown etiology. There are many reports stating that the sensitivity and specificity of QuantiFERON-tuberculosis (QFT) and sputum culture are low in latent tuberculosis infection of dialysis patients. Accordingly it is necessary to diagnose mycobacterium tuberculous peritonitis comprehensively by the clinical symptoms and image analysis.
100 项与 盐酸头孢替安酯 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 脓肿 | 日本 | 1990-01-01 | |
| 烧伤感染 | 日本 | 1990-01-01 | |
| 膀胱炎 | 日本 | 1990-01-01 | |
| 泪囊炎 | 日本 | 1990-01-01 | |
| 大肠杆菌感染 | 日本 | 1990-01-01 | |
| 嗜血杆菌感染 | 日本 | 1990-01-01 | |
| 感染 | 日本 | 1990-01-01 | |
| 角膜炎 | 日本 | 1990-01-01 | |
| 中耳炎 | 日本 | 1990-01-01 | |
| 肺炎球菌感染 | 日本 | 1990-01-01 | |
| 肺炎 | 日本 | 1990-01-01 | |
| 肾盂肾炎 | 日本 | 1990-01-01 | |
| 呼吸道感染 | 日本 | 1990-01-01 | |
| 鼻窦炎 | 日本 | 1990-01-01 | |
| 传染性皮肤病 | 日本 | 1990-01-01 | |
| 葡萄球菌感染 | 日本 | 1990-01-01 | |
| 口腔炎 | 日本 | 1990-01-01 | |
| 链球菌感染 | 日本 | 1990-01-01 | |
| 扁桃体炎 | 日本 | 1990-01-01 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 细菌感染 | 临床3期 | 中国 | 2015-09-11 | |
| 急性支气管炎 | 临床1期 | 中国 | 2014-09-04 | |
| 角膜溃疡 | 临床1期 | 中国 | 2014-09-04 | |
| 睑腺炎 | 临床1期 | 中国 | 2014-09-04 | |
| 喉炎 | 临床1期 | 中国 | 2014-09-04 | |
| 淋巴结炎 | 临床1期 | 中国 | 2014-09-04 | |
| 淋巴管炎 | 临床1期 | 中国 | 2014-09-04 | |
| 乳腺炎 | 临床1期 | 中国 | 2014-09-04 | |
| 肛周脓肿 | 临床1期 | 中国 | 2014-09-04 | |
| 脓皮症 | 临床1期 | 中国 | 2014-09-04 |
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